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AR046222A1 - PHARMACEUTICAL COMPOSITIONS OF SUSTAINED LIBERATION INCLUDING APLINDORE AND ITS DERIVATIVES - Google Patents

PHARMACEUTICAL COMPOSITIONS OF SUSTAINED LIBERATION INCLUDING APLINDORE AND ITS DERIVATIVES

Info

Publication number
AR046222A1
AR046222A1 ARP040103986A ARP040103986A AR046222A1 AR 046222 A1 AR046222 A1 AR 046222A1 AR P040103986 A ARP040103986 A AR P040103986A AR P040103986 A ARP040103986 A AR P040103986A AR 046222 A1 AR046222 A1 AR 046222A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
defined above
hydrogen
controlled release
Prior art date
Application number
ARP040103986A
Other languages
Spanish (es)
Original Assignee
Wyeth Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34572826&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR046222(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of AR046222A1 publication Critical patent/AR046222A1/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)

Abstract

Reivindicación 1: Una formulación de dosis de liberación controlada, caracterizada porque comprende un compuesto de la fórmula (1), en la cual: R1y R2 son, independientemente, hidrógeno, alquilo C1-6, fenilo o bencilo; o R1 y R2, tomados en conjunto, son bencilideno opcionalmente sustituido con R3 como se define más adelante o alquilideno de hasta 6 átomos de carbono; o R1 y R2, tomados en conjunto con el átomo de carbono al cual están unidos, forman un residuo carbonilo o un grupo cicloalquilo que tiene hasta 6 átomos de carbono; R3 es hidrógeno, hidroxi, halógeno, trifluorometilo, trifluorometoxi, alquilo C1-6, alcoxi C1-6, arilalcoxi C7-12, alcanoiloxi C2-6, amino, mono- o di-alquilamino en el cual cada grupo alquilo C1-6, alcanamido C2-6 o alcanosulfonamido C1-6; R4 es hidrógeno o alquilo C1-6; n es uno de los números enteros 0, 1, 2, 3, 4, 5, ó 6; Z es hidrógeno, hidroxi, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, cicloalquilo C3-8, alquilo policíclico C7-15, fenilo opcionalmente sustituido con R3 como se ha definido antes, fenoxi, opcionalmente sustituido con R3 como se ha definido antes, naftilo opcionalmente sustituido con R3 como se ha definido antes o naftiloxi opcionalmente sustituido con R3 como se ha definido antes, heteroarilo o heteroariloxi, en donde el anillo heterocíclico del grupo heteroarilo o heteroariloxi es seleccionado de tiofeno, furano, piridina, pirazina, pirimidina, indol, indazol imidazol, cromano, cumarina, carboestirilo, quinolina, bencisoxazol, benzoxazol, pirazol, pirrol, tiazol, oxazol, o isoxazol y el anillo heterocíclico está opcionalmente sustituido por R3 como se ha definido antes; o una sal farmacéuticamente aceptable de lo mismo. Reivindicación 22: Un método de tratamiento para un desorden del sistema dopaminérgico, caracterizado porque comprende administrar a un paciente que necesita de dicho tratamiento una formulación de dosis de liberación controlada de acuerdo a cualquiera de las reivindicaciones 1-21. Reivindicación 53: Un conjunto de formas de dosis de liberación controlada, caracterizado porque comprende una pluralidad de formas de dosis de liberación controlada individuales, en donde cada forma de dosis individual comprende una cantidad diferente de dicho compuesto de acuerdo a las reivindicaciones 1, 7 o 17.Claim 1: A controlled release dose formulation, characterized in that it comprises a compound of the formula (1), in which: R1 and R2 are, independently, hydrogen, C1-6 alkyl, phenyl or benzyl; or R1 and R2, taken together, are benzylidene optionally substituted with R3 as defined below or alkylidene of up to 6 carbon atoms; or R1 and R2, taken in conjunction with the carbon atom to which they are attached, form a carbonyl residue or a cycloalkyl group having up to 6 carbon atoms; R3 is hydrogen, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, C1-6 alkyl, C1-6 alkoxy, C7-12 arylalkoxy, C2-6 alkanoyloxy, amino, mono- or di-alkylamino in which each C1-6 alkyl group, C2-6 alkanamide or C1-6 alkanesulfonamido; R4 is hydrogen or C1-6 alkyl; n is one of the integers 0, 1, 2, 3, 4, 5, or 6; Z is hydrogen, hydroxy, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C3-8 cycloalkyl, C7-15 polycyclic alkyl, phenyl optionally substituted with R3 as defined above, phenoxy, optionally substituted with R3 as defined above, naphthyl optionally substituted with R3 as defined above or naphthyloxy optionally substituted with R3 as defined above, heteroaryl or heteroaryloxy, wherein the heterocyclic ring of the heteroaryl or heteroaryloxy group is selected from thiophene , furan, pyridine, pyrazine, pyrimidine, indole, indazol imidazole, chromane, coumarin, carbostyryl, quinoline, bencisoxazole, benzoxazole, pyrazole, pyrrole, thiazole, oxazole, or isoxazole and the heterocyclic ring is optionally substituted by R3 as defined above ; or a pharmaceutically acceptable salt thereof. Claim 22: A treatment method for a dopamine system disorder, characterized in that it comprises administering to a patient in need of said treatment a controlled release dose formulation according to any of claims 1-21. Claim 53: A set of controlled release dose forms, characterized in that it comprises a plurality of individual controlled release dose forms, wherein each individual dose form comprises a different amount of said compound according to claims 1, 7 or 17.

ARP040103986A 2003-10-29 2004-10-29 PHARMACEUTICAL COMPOSITIONS OF SUSTAINED LIBERATION INCLUDING APLINDORE AND ITS DERIVATIVES AR046222A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US51531503P 2003-10-29 2003-10-29

Publications (1)

Publication Number Publication Date
AR046222A1 true AR046222A1 (en) 2005-11-30

Family

ID=34572826

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040103986A AR046222A1 (en) 2003-10-29 2004-10-29 PHARMACEUTICAL COMPOSITIONS OF SUSTAINED LIBERATION INCLUDING APLINDORE AND ITS DERIVATIVES

Country Status (21)

Country Link
US (5) US20050095292A1 (en)
EP (1) EP1675583B1 (en)
JP (1) JP5547865B2 (en)
KR (1) KR101409724B1 (en)
CN (2) CN1874767A (en)
AR (1) AR046222A1 (en)
AU (1) AU2004286855B2 (en)
BR (1) BRPI0415953B8 (en)
CA (1) CA2543045C (en)
ES (1) ES2405404T3 (en)
GT (1) GT200400218A (en)
IL (1) IL174958A (en)
MX (1) MXPA06004752A (en)
NO (1) NO20062004L (en)
PA (1) PA8616201A1 (en)
PE (1) PE20050484A1 (en)
RU (1) RU2376988C2 (en)
SG (1) SG147450A1 (en)
TW (1) TW200517106A (en)
WO (1) WO2005044262A1 (en)
ZA (1) ZA200603409B (en)

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Also Published As

Publication number Publication date
JP2007509970A (en) 2007-04-19
PE20050484A1 (en) 2005-10-13
BRPI0415953B8 (en) 2021-05-25
AU2004286855B2 (en) 2011-04-21
US20180344695A1 (en) 2018-12-06
KR101409724B1 (en) 2014-06-19
US10292966B2 (en) 2019-05-21
MXPA06004752A (en) 2006-07-05
CN1874767A (en) 2006-12-06
CN102335116A (en) 2012-02-01
KR20060110281A (en) 2006-10-24
BRPI0415953B1 (en) 2018-12-26
ES2405404T3 (en) 2013-05-31
RU2376988C2 (en) 2009-12-27
BRPI0415953A (en) 2007-01-02
US20200138781A1 (en) 2020-05-07
IL174958A0 (en) 2008-04-13
GT200400218A (en) 2005-06-06
EP1675583B1 (en) 2013-02-27
US20230061743A1 (en) 2023-03-02
CA2543045C (en) 2013-12-17
US20180193311A1 (en) 2018-07-12
PA8616201A1 (en) 2005-05-24
IL174958A (en) 2012-08-30
JP5547865B2 (en) 2014-07-16
CA2543045A1 (en) 2005-05-19
TW200517106A (en) 2005-06-01
ZA200603409B (en) 2010-10-27
EP1675583A1 (en) 2006-07-05
US20050095292A1 (en) 2005-05-05
AU2004286855A1 (en) 2005-05-19
US10463648B2 (en) 2019-11-05
US11179369B2 (en) 2021-11-23
WO2005044262A1 (en) 2005-05-19
RU2006118321A (en) 2007-12-10
HK1089394A1 (en) 2006-12-01
NO20062004L (en) 2006-07-07
SG147450A1 (en) 2008-11-28

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